کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375628 | 981942 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors](/preview/png/1375628.png)
چکیده انگلیسی
In an effort to identify HDAC isoform selective inhibitors, we designed and synthesized novel, chiral 3,4-dihydroquinoxalin-2(1H)-one and piperazine-2,5-dione aryl hydroxamates showing selectivity (up to 40-fold) for human HDAC6 over other class I/IIa HDACs. The observed selectivity and potency (IC50 values 10–200 nM against HDAC6) is markedly dependent on the absolute configuration of the chiral moiety, and suggests new possibilities for use of chiral compounds in selective HDAC isoform inhibition.
A number of potent (IC50 = 10–200 nM) and highly selective HDAC6 inhibitors are reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 3, 1 February 2009, Pages 688–692
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 3, 1 February 2009, Pages 688–692
نویسندگان
David V. Smil, Sukhdev Manku, Yves A. Chantigny, Silvana Leit, Amal Wahhab, Theresa P. Yan, Marielle Fournel, Christiane Maroun, Zuomei Li, Anne-Marie Lemieux, Alina Nicolescu, Jubrail Rahil, Sylvain Lefebvre, Anthony Panetta, Jeffrey M. Besterman,